Recent advances of chroman-4-one derivatives: Synthetic approaches and bioactivities

•Chroman-4-one scaffold is a privileged structure in drug design and discovery.•Structural derivatization of chromanone was mainly focused on 2, 3 and 4-positions.•The main families include 3-benzylidene-chromanones, flavanones, and isoflavanones.•The 3-benzylidene-chromanone family was considered more extensively by researchers.•The flavanones and isoflavanones are related to the naturally occurring flavonoids.

Chroman-4-one scaffold is a privileged structure in heterocyclic chemistry and drug discovery. Also, chroman-4-ones are important intermediates and interesting building blocks in organic synthesis and drug design. The structural diversity found in the chroman-4-one family led to their division into several categories including benzylidene-4-chromanones, flavanones (2-phenyl-4-chromanones), isoflavanones (3-phenyl-4-chromanones), spirochromanones, and C-4 modified chroman-4-ones such as hydrazones and oxime derivatives. This review addresses the most significant synthetic methods reported on 4-chromanone-derived compounds and consequently emphasizes on the biological relevance of such compounds.

Graphical abstractChroman-4-ones are important intermediates and interesting building-blocks in organic synthesis and drug design. This review addresses the most significant synthetic methods and the biological relevance of 4-chromanone-derived compounds.Figure optionsDownload full-size imageDownload as PowerPoint slide